Loperamide is a synthetic opiate that efficiently and selectively activates the μ opioid receptors Ki = 0.16 nM, exclusively at the periphery. N-Desmethyl-loperamide (dLop) is the main metabolite of loperamide. dLop is a substrate of an ATP-dependent outflow conveyor, P-glycoprotein. As a result, both the initial compound and the mapping of metabolites, limited by passage through the blood, can be analyzed by various methods.
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